parasitemia

Fosravuconazole L-lysine ethanolate (BMS-379224 L-lysine ethanolate) 是一种口服广谱抗真菌剂，是Ravuconazole 的前药，可研究念珠菌病，灰指甲病和寄生虫病。

Piperaquine 是一种双喹啉抗疟化合物，是青蒿素的伴侣化合物。Piperaquine 是Eurartesim 的组成部分，常用于研究疟疾感染。

Moxipraquine 是一种新型的8-氨基喹诺酮类化合物，对克氏锥虫具有抗感染活性。Moxipraquine 能有效抑制寄生虫血症，但不能根除小鼠或豚鼠的感染。Moxipraquine 对重度利什曼原虫、墨西哥乳杆菌和巴西乳杆菌的实验性感染有效，但对巴西乳杆菌无效。

Violacein is a bacterial metabolite originally isolated from C. violaceum that has antibacterial and antiprotozoal activities.[1] [2] It is produced by C. violaceum as a purple pigment in response to N-hexanoyl homoserine lactone , a property that has been modified to create a strain of C. violaceum used in detecting quorum-sensing molecules.[3] Violacein is active against Gram-positive bacteria, including B. subtilis and S. aureus (MICs = 0.8 and 1.6 µM, respectively). It is also active against P. falciparum, including chloroquine-susceptible and -resistant strains (IC50s = 0.85 and 0.63 µM, respectively).[2] It reduces parasitemia in a mouse model of nonlethal P. chabaudi chabaudi infection when administered at a dose of 7.5 mg/kg and increases survival in a mouse model of lethal P. chabaudi chabaudi infection. Violacein permeabilizes the cytoplasmic membrane of bacterial cells but does not affect the cell wall.[1]

Purfalcamine is an orally active, selective Plasmodium falciparum calcium-dependent protein kinase 1 (PfCDPK1) inhibitor with an IC50 of 17 nM and an EC50 of 230 nM. Purfalcamine has antimalarial activity and causes malaria parasites developmental arrest at the schizont stage[1][2]. Purfalcamine has low activity against Toxoplasma gondii calcium-dependent protein kinase 3 (TgCDPK3)[1]. Purfalcamine (225, 450 nM) has no effect on the parasitemia in the first 32 hours. After about 40 hours, parasite level remains stable and then begins dropping[1]. Purfalcamine inhibits proliferation with EC50s of 171-259 nM for P. falciparum strains (3D7, Dd2, FCB, HB3 and W2), which indicates effectiveness against drug-resistant parasites[1]. Given that the EC50 value for P. falciparum (3D7) is 230 nM, Purfalcamine shows a therapeutic window ranging from 23-fold to 36-fold (EC50s for CHO=12.33 μM, HEp2=7.235 μM, HeLa=7.029 μM and Huh7=5.476 μM)[1]. Purfalcamine (10 mg kg; oral gavage; BID; for 6 days) demonstrates a delay in the onset of parasitemia in treated mice[1]. Purfalcamine (20 mg kg; orally gavage) exhibits a Cmax of 2.6 μM with a half-life of 3.1 hours[1]. Animal Model: Male BALB c mice, 7 weeks of age with the malaria parasite[1] [1]. Nobutaka Kato, et al. Gene expression signatures and small-molecule compounds link a protein kinase to Plasmodium falciparum motility. Nat Chem Biol. 2008 Jun;4(6):347-56. [2]. Rajshekhar Y Gaji, et al. Expression of the essential Kinase PfCDPK1 from Plasmodium falciparum in Toxoplasma gondii facilitates the discovery of novel antimalarial drugs. Antimicrob Agents Chemother. 2014 May;58(5):2598-607.

JMI-105 具有用作抗疟剂的潜力。JMI-105 是恶性疟原虫 -2 蛋白酶(PfFP-2)的有效抑制剂，可抑制恶性疟原虫菌株的CQS 株 (3D7) 和 CQR 株 (RKL-9) 的生长，IC50值分别为8.8 μM 和14.3 μM。在伯氏疟原虫 ANKA 感染小鼠模型中，JMI-105 显著降低寄生虫血症并延长宿主存活期。

SJ000025081 是一种二氢吡啶，能够用做抗疟剂。在小鼠疟疾模型中，SJ000025081 显著抑制 P. yoelii 感染的寄生虫血症。

FTI-2628 is a novel inhibitor of protein farnesyltransferase (FT), inhibiting the growth of P. falciparum in red blood cells and suppressing parasitemia.

Antimalarial agent 26是一种1,4-萘醌衍生物，作为口服抗疟药物，对恶性疟原虫(P. falciparum)表现出细胞毒性，并具有优于哺乳动物细胞系的选择性。该化合物能够有效抑制体内P. berghei引起的寄生虫血症。

Antimalarial agent 25是一种口服有效的1,4-萘醌衍生物，具有抗疟活性。Antimalarial agent 25显示出对P. falciparum的细胞毒性，并在体内抑制P. burghei诱导的寄生虫血症。